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targets (18) enzymes (2)
for drugs
Identification
Name Galantamine
Accession Number DB00674 (APRD00206, EXPT01628)
Type small molecule
Groups approved
Description

A benzazepine derived from norbelladine. It is found in galanthus and other amaryllidaceae. Galantamine is a cholinesterase inhibitor that has been used to reverse the muscular effects of gallamine triethiodide and tubocurarine, and has been studied as a treatment for Alzheimer’s disease and other central nervous system disorders. [PubChem]
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
(-)-Galanthamine
Galanthamine
Galanthamine hydrobromide
Salts Not Available
Brand names
Name Company
Galantamin
Jilkon
Lycoremin
Lycoremine
Reminyl
Brand mixtures Not Available
Categories
  • Parasympathomimetics
  • Cholinesterase Inhibitors
  • Nootropic Agents
CAS number 357-70-0
Weight Average: 287.3535
Monoisotopic: 287.152143543
Chemical Formula C17H21NO3
InChI Key InChIKey=ASUTZQLVASHGKV-JDFRZJQESA-N
InChI
InChI=1S/C17H21NO3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-6,12,14,19H,7-10H2,1-2H3/t12-,14-,17-/m0/s1
Plain Text
IUPAC Name
(1S,12S,14R)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.0^{1,12}.0^{6,17}]heptadeca-6,8,10(17),15-tetraen-14-ol
SMILES
[H][C@]12C[C@@H](O)C=C[C@]11CCN(C)CC3=C1C(O2)=C(OC)C=C3
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Organic
Classes
  • Benzofurans
  • Phenylpropylamines
Substructures
  • Benzofurans
  • Hydroxy Compounds
  • Alkanes and Alkenes
  • Phenols and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Catechols
  • Heterocyclic compounds
  • Aromatic compounds
  • Anisoles
  • Phenylpropylamines
  • Alcohols and Polyols
  • Cyclohexenes and Derivatives
  • Phenyl Esters
Pharmacology
Indication For the treatment of mild to moderate dementia of the Alzheimer's type. Has also been investigated in patients with mild cognitive impairment who did not meet the diagnostic criteria for Alzheimer's disease.
Pharmacodynamics Galantamine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. It is indicated for the treatment of mild to moderate dementia of the Alzheimer's type. An early pathophysiological feature of Alzheimer's disease that is associated with memory loss and cognitive deficits is a deficiency of acetylcholine as a result of selective loss of cholinergic neurons in the cerebral cortex, nucleus basalis, and hippocampus. Galantamine is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by acetylcholinesterase. If this proposed mechanism of action is correct, Galantamine's effect may lessen as the disease progresses and fewer cholinergic neurons remain functionally intact. There is no evidence that Galantamine alters the course of the underlying dementing process.
Mechanism of action Galantamine is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor. It is not structurally related to other acetylcholinesterase inhibitors. Galantamine's proposed mechanism of action involves the reversible inhibition of acetylcholinesterase, which prevents the hydrolysis of acetycholine, leading to an increased concentration of acetylcholine at cholinergic synapses. Galantamine also binds allosterically with nicotinic acetylcholine receptors and may possibly potentiate the action of agonists (such as acetylcholine) at these receptors.
Absorption Not Available
Volume of distribution
  • 175 L
Protein binding 18%
Metabolism Not Available
Route of elimination Galantamine is metabolized by hepatic cytochrome P450 enzymes, glucuronidated, and excreted unchanged in the urine.
Half life 7 hours
Clearance
  • 300 mL/min [After IV. or oral administration]
Toxicity LD50=75 mg/kg (rat)
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers
  • Barr laboratories inc
  • Impax laboratories inc
  • Watson laboratories inc
  • Ortho mcneil janssen pharmaceuticals inc
  • Roxane laboratories inc
  • Ortho mcneil janssen pharmaceutical inc
  • Actavis elizabeth llc
  • Beijing yabao biopharmaceutical co ltd
  • Dr reddys laboratories ltd
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa
Packagers
Dosage forms
Form Route Strength
Capsule, extended release Oral
Tablet Oral
Prices
Unit description Cost Unit
Galantamine Hydrobromide 30 16 mg 24 Hour Capsule Bottle 198.58 USD bottle
Galantamine Hydrobromide 30 8 mg 24 Hour Capsule Bottle 198.58 USD bottle
Razadyne 12 mg tablet 8.3 USD tablet
Razadyne 4 mg tablet 5.36 USD tablet
Razadyne 8 mg tablet 3.66 USD tablet
Galantamine hbr 12 mg tablet 3.18 USD tablet
Galantamine hbr 4 mg tablet 3.18 USD tablet
Galantamine hbr 8 mg tablet 3.18 USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Country Patent Number Approved Expires (estimated)
United States 7160559 1999-12-20 2019-12-20
United States 6099863 1997-06-06 2017-06-06
Canada 2358062 2006-12-19 2019-12-20
Canada 2310926 2001-11-20 2017-06-06
Properties
State solid
Experimental Properties
Property Value Source
melting point 269-270 °C (HBr salt) Not Available
water solubility 10 mg/mL (HBr salt) Not Available
logP 1.8 Not Available
Predicted Properties
Property Value Source
water solubility 1.70e+00 g/l ALOGPS
logP 1.39 ALOGPS
logP 1.16 ChemAxon
logS -2.2 ALOGPS
pKa (strongest acidic) 14.81 ChemAxon
pKa (strongest basic) 8.91 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 4 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 41.93 ChemAxon
rotatable bond count 1 ChemAxon
refractivity 82.3 ChemAxon
polarizability 31.4 ChemAxon
References
Synthesis Reference Not Available
General Reference
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Greenblatt HM, Kryger G, Lewis T, Silman I, Sussman JL: Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution. FEBS Lett. 1999 Dec 17;463(3):321-6. Pubmed
  3. Woodruff-Pak DS, Vogel RW 3rd, Wenk GL: Galantamine: effect on nicotinic receptor binding, acetylcholinesterase inhibition, and learning. Proc Natl Acad Sci U S A. 2001 Feb 13;98(4):2089-94. Epub 2001 Feb 6. Pubmed
  4. Birks J: Cholinesterase inhibitors for Alzheimer’s disease. Cochrane Database Syst Rev. 2006 Jan 25;(1):CD005593. Pubmed# Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  5. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed# Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
External Links
Resource Link
KEGG Drug D04292 Link_out
KEGG Compound C08526 Link_out
PubChem Compound 908828 Link_out
PubChem Substance 46505659 Link_out
ChemSpider 23175565 Link_out
BindingDB 10404 Link_out
ChEBI 5264 Link_out
ChEMBL 5264 Link_out
Therapeutic Targets Database DAP000559 Link_out
PharmGKB PA449726 Link_out
HET GNT Link_out
Drug Product Database 2266717 Link_out
RxList http://www.rxlist.com/cgi/generic/reminyl.htm Link_out
Drugs.com http://www.drugs.com/cdi/galantamine.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Galantamine Link_out
ATC Codes
  • N06DA04
AHFS Codes
  • 12:04.00
PDB Entries Not Available
FDA label show (278 KB)
MSDS show (28.4 KB)
Interactions
Drug Interactions
Drug Interaction
Acepromazine Possible antagonism of action
Aceprometazine Possible antagonism of action
Alverine Possible antagonism of action
Amantadine Possible antagonism of action
Amitriptyline Possible antagonism of action
Amoxapine Possible antagonism of action
Atropine Possible antagonism of action
Azatadine Possible antagonism of action
Benzatropine Possible antagonism of action
Biperiden Possible antagonism of action
Brompheniramine Possible antagonism of action
Carbinoxamine Possible antagonism of action
Chlorpheniramine Possible antagonism of action
Chlorpromazine Possible antagonism of action
Chlorprothixene Possible antagonism of action
Cimetidine Possible antagonism of action
Clemastine Possible antagonism of action
Clidinium Possible antagonism of action
Clomipramine Possible antagonism of action
Clozapine Possible antagonism of action
Cyclizine Possible antagonism of action
Cyclobenzaprine Possible antagonism of action
Cyproheptadine Possible antagonism of action
Darifenacin Possible antagonism of action
Desipramine Possible antagonism of action
Dexbrompheniramine Possible antagonism of action
Dicyclomine Possible antagonism of action
Dimenhydrinate Possible antagonism of action
Diphenhydramine Possible antagonism of action
Diphenoxylate Possible antagonism of action
Diphenylpyraline Possible antagonism of action
Disopyramide Possible antagonism of action
Doxepin Possible antagonism of action
Doxylamine Possible antagonism of action
Ethopropazine Possible antagonism of action
Flavoxate Possible antagonism of action
Flupenthixol Possible antagonism of action
Glutethimide Possible antagonism of action
Glycopyrrolate Possible antagonism of action
Hydroxyzine Possible antagonism of action
Hyoscyamine Possible antagonism of action
Imipramine Possible antagonism of action
Isocarboxazid Possible antagonism of action
Isopropamide Possible antagonism of action
Ketoconazole Ketoconazole increases the effect and toxicity of galantamine
Loxapine Possible antagonism of action
Maprotiline Possible antagonism of action
Meclizine Possible antagonism of action
Meperidine Possible antagonism of action
Mesoridazine Possible antagonism of action
Methdilazine Possible antagonism of action
Methotrimeprazine Possible antagonism of action
Methylscopolamine Possible antagonism of action
Mirtazapine Possible antagonism of action
Moclobemide Possible antagonism of action
Molindone Possible antagonism of action
Nortriptyline Possible antagonism of action
Olanzapine Possible antagonism of action
Orphenadrine Possible antagonism of action
Oxybutynin Possible antagonism of action
Paroxetine Paroxetine increases the effect and toxicity of galantamine
Perphenazine Possible antagonism of action
Phenelzine Possible antagonism of action
Phenindamine Possible antagonism of action
Pimozide Possible antagonism of action
Pipotiazine Possible antagonism of action
Procainamide Possible antagonism of action
Prochlorperazine Possible antagonism of action
Procyclidine Possible antagonism of action
Promazine Possible antagonism of action
Promethazine Possible antagonism of action
Propantheline Possible antagonism of action
Propericiazine Possible antagonism of action
Protriptyline Possible antagonism of action
Quetiapine Possible antagonism of action
Quinidine Possible antagonism of action
Quinidine barbiturate Possible antagonism of action
Risperidone Possible antagonism of action
Scopolamine Possible antagonism of action
Sertraline Possible antagonism of action
Solifenacin Possible antagonism of action
Thioproperazine Possible antagonism of action
Thioridazine Possible antagonism of action
Thiothixene Possible antagonism of action
Tizanidine Possible antagonism of action
Tolterodine Possible antagonism of action
Tranylcypromine Possible antagonism of action
Trazodone Possible antagonism of action
Trifluoperazine Possible antagonism of action
Triflupromazine Possible antagonism of action
Trihexyphenidyl Possible antagonism of action
Trimeprazine Possible antagonism of action
Trimethobenzamide The therapeutic effects of the anticholinergic, Trimethobenzamide, and/or the acetylcholinesterase inhibitor (central), Galantamine, may be reduced due to antagonism. Monitor therapeutic effects of both agents.
Trimipramine Possible antagonism of action
Tripelennamine Possible antagonism of action
Triprolidine Possible antagonism of action
Trospium The therapeutic effects of the anticholinergic, Trospium, and/or the acetylcholinesterase inhibitor (central), Galantamine, may be reduced due to antagonism. Monitor therapeutic effects of both agents.
Ziprasidone Possible antagonism of action
Zuclopenthixol Possible antagonism of action
Food Interactions
  • Take with food.
Targets

1. Acetylcholinesterase

Pharmacological action: yes
Actions: inhibitor

Rapidly hydrolyzes choline released into the synapse

Organism class: human
UniProt ID: P22303 Link_out
Gene: ACHE Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Tonkopii VD, Prozorovskii VB, Suslova IM: [Interaction of reversible inhibitors with the catalytic centers and allosteric sites of cholinesterases] Biull Eksp Biol Med. 1976 Aug;82(8):947-50. Pubmed
  2. Greenblatt HM, Kryger G, Lewis T, Silman I, Sussman JL: Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution. FEBS Lett. 1999 Dec 17;463(3):321-6. Pubmed
  3. Guillou C, Mary A, Renko DZ, Gras E, Thal C: Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts. Bioorg Med Chem Lett. 2000 Apr 3;10(7):637-9. Pubmed
  4. Blesa R: Galantamine: therapeutic effects beyond cognition. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:28-34. Pubmed
  5. Stahl SM: The new cholinesterase inhibitors for Alzheimer’s disease, Part 1: their similarities are different. J Clin Psychiatry. 2000 Oct;61(10):710-1. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  7. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  8. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed# Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  9. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  10. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  11. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed
  12. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed

2. Acetylcholine receptor subunit alpha

Pharmacological action: unknown
Actions: allosteric modulator
UniProt ID: P02708 Link_out
Gene: CHRNA1
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

3. Acetylcholine receptor subunit beta

Pharmacological action: unknown
Actions: allosteric modulator
UniProt ID: P11230 Link_out
Gene: CHRNB1
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

4. Acetylcholine receptor subunit delta

Pharmacological action: unknown
Actions: allosteric modulator
UniProt ID: Q07001 Link_out
Gene: CHRND
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

5. Acetylcholine receptor subunit gamma

Pharmacological action: unknown
Actions: allosteric modulator
UniProt ID: P07510 Link_out
Gene: CHRNG
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

6. Acetylcholine receptor subunit epsilon

Pharmacological action: unknown
Actions: allosteric modulator
UniProt ID: Q04844 Link_out
Gene: CHRNE
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

7. Neuronal acetylcholine receptor subunit alpha-2

Pharmacological action: unknown
Actions: allosteric modulator

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane

Organism class: human
UniProt ID: Q15822 Link_out
Gene: CHRNA2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

8. Neuronal acetylcholine receptor subunit alpha-3

Pharmacological action: unknown
Actions: allosteric modulator

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane

Organism class: human
UniProt ID: P32297 Link_out
Gene: CHRNA3 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

9. Neuronal acetylcholine receptor subunit alpha-4

Pharmacological action: unknown
Actions: allosteric modulator

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane

Organism class: human
UniProt ID: P43681 Link_out
Gene: CHRNA4 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

10. Neuronal acetylcholine receptor subunit alpha-5

Pharmacological action: unknown
Actions: allosteric modulator

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane

Organism class: human
UniProt ID: P30532 Link_out
Gene: CHRNA5 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

11. Neuronal acetylcholine receptor subunit alpha-6

Pharmacological action: unknown
Actions: allosteric modulator

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane

Organism class: human
UniProt ID: Q15825 Link_out
Gene: CHRNA6 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

12. Neuronal acetylcholine receptor subunit alpha-7

Pharmacological action: unknown
Actions: allosteric modulator

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane

Organism class: human
UniProt ID: P36544 Link_out
Gene: CHRNA7 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

13. Neuronal acetylcholine receptor subunit alpha-9

Pharmacological action: unknown
Actions: allosteric modulator

Ionotropic receptor with a probable role in the modulation of auditory stimuli. Agonist binding may induce an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane. In the ear, this may lead to a reduction in basilar membrane motion, altering the activity of auditory nerve fibers and reducing the range of dynamic hearing. This may protect against acoustic trauma. May also regulate keratinocyte adhesion

Organism class: human
UniProt ID: Q9UGM1 Link_out
Gene: CHRNA9 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

14. Neuronal acetylcholine receptor subunit alpha-10

Pharmacological action: unknown
Actions: allosteric modulator

Ionotropic receptor with a probable role in the modulation of auditory stimuli. Agonist binding may induce an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane. In the ear, this may lead to a reduction in basilar membrane motion, altering the activity of auditory nerve fibers and reducing the range of dynamic hearing. This may protect against acoustic trauma

Organism class: human
UniProt ID: Q9GZZ6 Link_out
Gene: CHRNA10 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

15. Neuronal acetylcholine receptor subunit beta-2

Pharmacological action: unknown
Actions: allosteric modulator

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane

Organism class: human
UniProt ID: P17787 Link_out
Gene: CHRNB2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

16. Neuronal acetylcholine receptor subunit beta-3

Pharmacological action: unknown
Actions: allosteric modulator

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane

Organism class: human
UniProt ID: Q05901 Link_out
Gene: CHRNB3 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

17. Neuronal acetylcholine receptor subunit beta-4

Pharmacological action: unknown
Actions: allosteric modulator

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane

Organism class: human
UniProt ID: P30926 Link_out
Gene: CHRNB4 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer’s disease. Drugs. 2000 Nov;60(5):1095-122. Pubmed
  2. Lilienfeld S: Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer’s disease. CNS Drug Rev. 2002 Summer;8(2):159-76. Pubmed
  3. Olin J, Schneider L: Galantamine for Alzheimer’s disease. Cochrane Database Syst Rev. 2002;(3):CD001747. Pubmed
  4. Lilienfeld S, Parys W: Galantamine: additional benefits to patients with Alzheimer’s disease. Dement Geriatr Cogn Disord. 2000 Sep;11 Suppl 1:19-27. Pubmed
  5. Woodruff-Pak DS, Lander C, Geerts H: Nicotinic cholinergic modulation: galantamine as a prototype. CNS Drug Rev. 2002 Winter;8(4):405-26. Pubmed
  6. Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Pubmed

18. Cholinesterase

Pharmacological action: unknown
Actions: inhibitor

An acylcholine + H(2)O = choline + a carboxylate

Organism class: human
UniProt ID: P06276 Link_out
Gene: BCHE Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Svoboda Z, Kvetina J, Kunesova G, Herink J, Bajgar J, Bartosova L, Zivny P, Palicka V: Effect of galantamine on acetylcholinesterase and butyrylcholinesterase activities in the presence of L-carnitine in rat selected brain and peripheral tissues. Neuro Endocrinol Lett. 2006 Dec;27 Suppl 2:183-6. Pubmed
  2. Giacobini E: Selective inhibitors of butyrylcholinesterase: a valid alternative for therapy of Alzheimer’s disease? Drugs Aging. 2001;18(12):891-8. Pubmed
  3. Wilkinson DG: Galantamine: a new treatment for Alzheimer’s disease. Expert Rev Neurother. 2001 Nov;1(2):153-9. Pubmed
Enzymes

1. Cytochrome P450 3A4

Actions: substrate

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4- hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. The enzyme also hydroxylates etoposide

UniProt ID: P08684 Link_out
Gene: CYP3A4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 2D6

Actions: substrate

Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants

UniProt ID: P10635 Link_out
Gene: CYP2D6 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
Comments
Drug created on June 13, 2005 07:24 / Updated on February 08, 2013 16:19